Albamycin NOVOBIOCIN BDBM50423645 Cathomycin
BDBM282 Coumarin-Based, DNA Gyrase Inhibitor (3R,4S,5R,6R)-5-hydroxy-6-[(2-hydroxy-3-{[4-hydroxy-3-(3-methylbut-2-en-1-yl)benzene]amido}-8-methyl-4-oxo-4H-chromen-7-yl)oxy]-3-methoxy-2,2-dimethyloxan-4-yl carbamate Novobiocin US20230364057, Compound Novobiocin
CHEMBL36506 Carbamic acid 5-hydroxy-6-{4-hydroxy-3-[4-hydroxy-3-(3-methyl-but-2-enyl)-benzoylamino]-8-methyl-2-oxo-2H-chromen-7-yloxy}-3-methoxy-2,2-dimethyl-tetrahydro-pyran-4-yl ester(Novobiocin) NOVOBIOCIN (3R,4S,5R,6R)-5-hydroxy-6-(4-hydroxy-3-(4-hydroxy-3-(3-methylbut-2-enyl)benzamido)-8-methyl-2-oxo-2H-chromen-7-yloxy)-3-methoxy-2,2-dimethyl-tetrahydro-2H-pyran-4-yl carbamate Carbamic acid 5-hydroxy-6-{4-hydroxy-3-[4-hydroxy-3-(3-methyl-but-2-enyl)-benzoylamino]-8-methyl-2-oxo-2H-chromen-7-yloxy}-3-methoxy-2,2-dimethyl-tetrahydro-pyran-4-yl ester Carbamic acid (3R,4S,5R,6R)-5-hydroxy-6-{4-hydroxy-3-[4-hydroxy-3-(4-methyl-pent-3-enyl)-benzoylamino]-8-methyl-2-oxo-2H-chromen-7-yloxy}-3-methoxy-2,2-dimethyl-tetrahydro-pyran-4-yl ester (3R,4S,5R,6R)-5-hydroxy-6-(4-hydroxy-3-(4-hydroxy-3-(3-methylbut-2-enyl)benzamido)-2-oxo-2H-chromen-7-yloxy)-3-methoxy-2,2-dimethyl-tetrahydro-2H-pyran-4-yl carbamate BDBM50226181 Carbamic acid (3R,4S,5R,6R)-5-hydroxy-6-{4-hydroxy-3-[4-hydroxy-3-(3-methyl-but-2-enyl)-benzoylamino]-8-methyl-2-oxo-2H-chromen-7-yloxy}-3-methoxy-2,2-dimethyl-tetrahydro-pyran-4-yl ester
- Zhao, H; Moroni, E; Yan, B; Colombo, G; Blagg, BS 3D-QSAR Assisted Design, Synthesis and Evaluation of Novobiocin Analogues. ACS Med Chem Lett 4: 57-62 (2012)
- Schio, L; Chatreaux, F; Loyau, V; Murer, M; Ferreira, A; Mauvais, P; Bonnefoy, A; Klich, M Fine Tuning of physico-chemical parameters to optimise a new series of novobiocin analogues. Bioorg Med Chem Lett 11: 1461-4 (2001)
- Peterson, LB; Blagg, BS Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues. Bioorg Med Chem Lett 20: 3957-60 (2010)
- Gunaherath, GM; Marron, MT; Wijeratne, EM; Whitesell, L; Gunatilaka, AA Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors. Bioorg Med Chem 21: 5118-29 (2013)
- GyraseB Assay Initially, equimolar quantities of about 0.5µM each of E. coli gyraseA and S. aureus gyraseB were incubated for a period of 45 min with salmon sperm DNA (Sigma) in 50mM Tris (pH 7.5), 75mM ammonium acetate buffer for the reconstitution of the hybrid topoisomerases at 4 OC. Later the assay was performed in a 96-well microtiter plate as mentioned earlier (7). The assay buffer includes 50 mM Tris (pH 7.5), 75 mM ammonium acetate, 5% w/v glycerol, 0.5mM ΕDTA, 6 mM magnesiumchloride, 0.001% Triton X-100, 1 mMdithiothreitol, DNA of 2 μg/mL (~3 μM base pairs), 250µM ATP, 2.2nM of E. coligyrase A and S. aureusgyraseB. Reactions were performed with various drug concentration ranges for the calculation of IC50, with a negative moxifloxacin and positive novobiocin control as standards. The reaction was allowed to proceed for 60 min and was quenched by addition of 20uL of malachite green reagent (POMG-25H, Bioassay systems, USA) subsequently absorbance was read at 650nm after 20 mi
- Supercoiling Assay Supercoiling assay was performed using the commercially available kit (DNA gyrase supercoiling assay kit: SAS4001) from Inspiralis Pvt.limited, Norwich, UK. The assay was performed in 1.5 mL eppendorf tubes at room temperature. According to the assay protocol, 1 U of S. aureus DNA gyrase was incubated with 0.5 µg of relaxed pBR 322 DNA in 30 µL reaction volume at 37oC for 30 min with 40 mM HEPES. KOH (pH 7.6), 10 mM magnesium acetate, 10 mM DTT, 2 mM ATP, 500 mM potassium glutamate, 0.05 mg/mL albumin (BSA). While the standard compound novobiocin was the positive control, 4% DMSO was considered as negative control. Subsequently, each reaction was stopped by the addition of 30 µL of Stop dye [40% sucrose, 100 mM Tris-HCl (pH 7.5), 1 mM EDTA and 0.5 mg/mL bromophenol blue] (8), briefly centrifuged for 45 sec and was run in 1% agarose gel in 1X TAE buffer (40mM Tris acetate, 2mM EDTA).